Neurotensin-Based Radioligands for NTS1R-Targeted Cancer Theranostics: Background, Current Status and Future Trends

Background/Objectives: The neurotensin subtype-1 receptor (NTS1R) is overexpressed in a number of human tumors, representing a valid biomolecular target for neurotensin-based radionuclide carriers. The latter are designed to deposit diagnostic–therapeutic radionuclides specifically on cancer lesions. This review summarizes research efforts toward the development, preclinical evaluation and first clinical outcomes of neurotensin-based radioligands in the diagnosis and therapy—radiotheranostics—of NTS1R-positive cancer.

Methods

The preclinical and few clinical studies related to NTS1R-targeted radiotheranostics are discussed. The crucial issue of in vivo metabolic stability is highlighted.

Results

Much effort has been dedicated to the development of effective NTS1R-directed radioligands for cancer theranostics, most of which are peptide-based. However, clinical success has been sub-optimal thus far, partly as a result of their fast degradation in the biological milieu.